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Galeterone (developmental code names TOK-001, VN/124-1) is a novel steroid antiandrogen that was under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique dual mechanism of action, acting as both an androgen receptor antagonist and a CYP17A1 inhibitor, the latter of which prevents the biosynthesis of androgens. As a CYP17A1 inhibitor, galeterone shows selectivity for 17,20-lyase over 17α-hydroxylase.
Galeterone was being compared to enzalutamide in a phase III clinical trial (ARMOR3-SV) for AR-V7-expressing metastatic castration-resistant prostate cancer. Tokai announced the discontinuation of ARMOR3-SV on July 26, 2016, after a data monitoring committee determined that the trial was unlikely to meet its endpoint. On August 22, 2016, the company announced the discontinuation of their phase II expansion (ARMOR2) as well.
In the week following cancellation of the ARMOR3-SV clinical trial, Tokai announced a reduction of its workforce by around 60% to a total of 10 "full-time equivalent employees." On December 22, 2016, a definitive share purchase agreement was announced, under which shareholders of Otic Pharma Ltd. would become the majority owners of Tokai Pharmaceuticals Inc., resulting in a NASDAQ-listed company (OticPharma, Inc.) focused on the development and commercialization of products for ear, nose, and throat disorders.
In August 2017, the development of galeterone was discontinued.
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